Acetaminophen Powder CAS 103-90-2

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  • Appearance: White powder
  • Assay: 99. 0%min
  • Stock: In stock
  • Sample: Available
  • Zhishang Chemical: Acetaminophen Supplement

Basic Info of Acetaminophen Powder

What is Acetaminophen Powder?

The chemical name of acetaminophen powder is N-(4-hydroxyphenyl)acetamide (N-(4-Hydroxyphenyl)acetamide). It became an over-the-counter drug in the United States in 1955, and began to be produced in my country in the late 1950s. Its appearance is white crystal or crystalline powder, melting point is 168~172℃, odorless, slightly bitter taste, easily soluble in hot water or ethanol, soluble in acetone, almost insoluble in cold water and petroleum ether. Stable below 45°C, but if exposed to humid air, it will be hydrolyzed into p-aminophenol, then further oxidized, and the color will gradually become pink, brown, and finally black, so it should be stored in a cool, dry place.

Acetaminophen powder plays an antipyretic effect by inhibiting the synthesis of prostaglandins in the hypothalamus thermoregulatory center, and its antipyretic effect is similar to aspirin. It produces analgesic effect, which is weaker than aspirin, and has few advantages such as allergic reactions. Increase.

Clinically, it is mainly used for fever, headache and relieve mild and moderate pain caused by colds, such as joint pain, muscle pain, neuralgia, migraine, dysmenorrhea, cancer pain and postoperative analgesia, etc. It can also be used for aspirin treatment. Patients who are allergic, intolerant or unsuitable for aspirin: such as chickenpox, hemophilia and other bleeding disorders (including those on anticoagulant therapy), and patients with mild peptic ulcers and gastritis; in addition, it can also be used It is used in the synthesis of the drug paramethadol, as an intermediate in organic synthesis, as a stabilizer for photographic chemicals and hydrogen peroxide.

Paracetamol Uses

  1. Acetaminophen, a phenolic organic substance, is utilized for fever triggered by the cold or flu, and is also utilized to relieve moderate to moderate pain such as migraine, joint discomfort, migraine, toothache, muscle pain, neuralgia, and dysmenorrhea.
  2. Acetaminophen can be used in patients who are allergic, intolerant, or unsuitable for aspirin: such as chickenpox, hemophilia, and other bleeding disorders (including those on anticoagulant therapy).
  3. Organic synthesis intermediates, stabilizers for hydrogen peroxide, photographic chemicals, non-anti-inflammatory antipyretic analgesics.
  4. Acetaminophen is used for fever reduction in people of all ages. The World Health Organization recommends using acetaminophen for cooling only when children have a fever above 38.5 °C (101.3 °F). The efficacy of acetaminophen in reducing fever in children has been questioned, and a meta-analysis has pointed out that acetaminophen is less effective in children than ibuprofen.
  5. Acetaminophen can be used to relieve pain.

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Pharmacological Action of Acetaminophen Powder

Paracetamol is an acetanilide antipyretic and analgesic drug, which is a metabolite of phenacetin in the body. Its analgesic mechanism is not very clear, it may be by inhibiting the synthesis of prostaglandins in the central nervous system (including inhibition of prostaglandin synthase) And block the impulse of pain nerve endings to produce analgesic effect. Its effect of blocking the impulse of pain nerve endings may be related to the inhibition of the synthesis of prostaglandins or other substances that can sensitize pain receptors (such as serotonin, bradykinin, etc.). Paracetamol can play an antipyretic effect by affecting the hypothalamus thermoregulatory center, which may be related to the inhibition of prostaglandin synthesis in the hypothalamus. Paracetamol has a strong antipyretic effect, similar to aspirin, and is more durable, but its analgesic and anti-inflammatory effects are weak, and it is ineffective against rheumatism at lower doses.

This is because paracetamol has a strong inhibitory effect on the synthesis and release of prostaglandins in the dorsal thalamus, while it has a weak inhibitory effect on the synthesis and release of peripheral prostaglandins. Therefore, paracetamol cannot replace aspirin or other non-steroidal anti-inflammatory drugs in the treatment of various types of arthritis, but can be used in cases of aspirin allergy, intolerance or inappropriate use of aspirin, such as chickenpox, hemophilia and other bleeding disorders ( Including the application of anticoagulant therapy), as well as peptic ulcer, gastritis, etc. Treat with paracetamol and, if necessary, other therapies to relieve the cause of pain or fever. Aspirin drugs (such as aspirin, paracetamol, ibuprofen, etc.) have protective effects to prevent cataracts.

Preparation of Acetaminophen Powder

Method 1: Add p-aminophenol to dilute acetic acid, then add glacial acetic acid, heat up to 150 °C for 7 hours, add acetic anhydride, and react for 2 hours, check the end point, after passing the test, cool down to below 25 °C, filter, and wash with water until no ethyl alcohol is present. Sour, dry, get a crude product.

Method 2: Distill p-aminophenol, glacial acetic acid and the acid mother liquor containing more than 50% acid together, and the speed of distilling out dilute acid is one-tenth of the total amount distilled per hour. Sampling to check that the residual content of p-aminophenol is less than 2.5%, add dilute acid (more than 50% content), and crystallize by cooling. The filtrate was filtered, washed with a small amount of dilute acid first, and then washed with a large amount of water until the filtrate was nearly colorless to obtain a crude product.

Method 1 yields 90% and method 2 yields 90-95%.

Refining method: When the water is heated to near boiling, it is put into the crude product. Warm up to complete dissolution, add activated carbon soaked in water, adjust to pH=4.2-4.6 with dilute acetic acid, and boil for 10min. Filter by pressure, add a small amount of sodium bisulfite to the filtrate. Cool to below 20°C to precipitate crystals. Filtering, washing and drying to obtain the finished product of the crude drug paracetamol.

Other production methods include: (1) reduction of p-nitrophenol with zinc in glacial acetic acid, and simultaneous acetylation to obtain paracetamol; (2) hydrazone generated by p-hydroxyacetophenone, placed in an acidic solution of sulfuric acid , adding sodium nitrite, translocation generates acetaminophen.

Reference

  1. Acetaminophen Monograph for Professionals. Drugs.com. [2020-10-24]
  2. Baby paracetamol asthma concernBBC News. 2008-09-19 [2020-10-24]
  3. State Pharmacopoeia Commission. Pharmacopoeia of the People’s Republic of China: 2010 Edition: First Supplement [M]. Beijing: China Pharmaceutical Science and Technology Press, 2010.

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